In the Pipeline/home/corante/public_html/pipeline/
en-usderekb.lowe@gmail.com2015-07-22T06:13:26-05:00hourly12000-01-01T12:00+00:00Chemical Probe Compounds: Time to Get Realhttp://pipeline.corante.com/archives/2015/07/22/chemical_probe_compounds_time_to_get_real.php
There's a new paper on chemical probes out in Nature Chemical Biology, and right off, I have to disclose a conflict of interest. I'm a co-author, and I'm glad to be one. (Here's a comment at Nature News, and here's...77838@/home/corante/public_html/pipeline/Chemical News2015-07-22T06:13:26-05:00Lipids, Proteins, and Chapman's Homerhttp://pipeline.corante.com/archives/2015/07/01/lipids_proteins_and_chapmans_homer.php
Longtime readers might recall that every so often I hit on the topic of the "dark matter" of drug target space. We have a lot of agents that hit G-protein coupled receptor proteins, and plenty that inhibit enzymes. Those, though,...77821@/home/corante/public_html/pipeline/Drug Assays2015-07-01T07:02:56-05:00PROTAC Goes Small-Moleculehttp://pipeline.corante.com/archives/2015/06/16/protac_goes_smallmolecule.php
Since I mentioned the Bradner lab's protein-destruction technology recently, I should also highlight this recent paper from Craig Crews and co-workers. In that post, I noted that their PROTAC method has been heading in a small-molecule direction, and this paper...77796@/home/corante/public_html/pipeline/Chemical Biology2015-06-16T11:27:18-05:00Targeting Proteins for Destructionhttp://pipeline.corante.com/archives/2015/05/26/targeting_proteins_for_destruction.php
Here's an excellent new paper that's appeared in the preprint area of Science, Science Express. Jay Bradner and co-workers at Harvard/Dana-Farber report a new way to control protein function, and this one seems both very effective and startlingly simple. The...77760@/home/corante/public_html/pipeline/Chemical Biology2015-05-26T06:11:26-05:00Controlling Proteins, One by Onehttp://pipeline.corante.com/archives/2015/05/20/controlling_proteins_one_by_one.php
Here's what looks like a very useful method for turning protein function on and off, reported in a new paper in Nature Chemistry. (This PDF link may work for you). The authors, from the MRC Molecular Biology labs at Cambridge...77756@/home/corante/public_html/pipeline/Chemical Biology2015-05-20T06:30:44-05:00Aileron and p53http://pipeline.corante.com/archives/2015/05/01/aileron_and_p53.php
In the long-running saga of getting a stapled peptide to work as a drug, Aileron Therapeutics was last heard from raising money for their p53 candidate. Now comes word that the company is basically going all-in with that one, raising...77727@/home/corante/public_html/pipeline/Cancer2015-05-01T06:30:16-05:00A New Dual DNA-Encoded Library Screenhttp://pipeline.corante.com/archives/2015/02/06/a_new_dual_dnaencoded_library_screen.php
I've written several times about DNA-encoded chemical libraries. Now comes an interesting new variation on them from Dario Neri and Jörg Scheurmann of the ETH in Zürich, pioneers in this area. As you can see from that scheme, what they're...77581@/home/corante/public_html/pipeline/Chemical Biology2015-02-06T07:50:00-05:00A New Cell Assay -And What It Says About Stapled Peptideshttp://pipeline.corante.com/archives/2015/01/20/a_new_cell_assay_and_what_it_says_about_stapled_peptides.php
I'm always looking out for new assays that might tell us what the heck is going on inside cells, so this paper caught my eye. The authors describe a new luciferase-based complementation assay for detecting protein-protein interactions. There are several...77547@/home/corante/public_html/pipeline/Drug Assays2015-01-20T07:10:11-05:00More Odd Compoundshttp://pipeline.corante.com/archives/2015/01/07/more_odd_compounds.php
When you look into the literature on small-molecule agents for really tricky targets, something stands out to medicinal chemists immediately: the structures start to get strange. Examples of this sort of thing are beyond counting, but this recent paper will...77528@/home/corante/public_html/pipeline/Academia (vs. Industry)2015-01-07T07:07:02-05:00Phage-Derived Catalystshttp://pipeline.corante.com/archives/2014/11/14/phagederived_catalysts.php
I've been enjoying this recent paper in JACS, but then I always like to see intersections of molecular biology with organic synthesis. The authors, from CUNY and the University of Strathclyde, are using a phage display library to see if...77448@/home/corante/public_html/pipeline/Chemical Biology2014-11-14T07:07:44-05:00Different Screening, Different Thermodynamics?http://pipeline.corante.com/archives/2014/10/17/different_screening_different_thermodynamics.php
Chris Lipinski and the folks at Collaborative Drug Discovery send word of an interesting webinar that will take place this coming Wednesday (October 22nd) at 2 PM EST. It's on enthalpic and entropic trends in ligand binding, and how various...77391@/home/corante/public_html/pipeline/Drug Assays2014-10-17T06:57:19-05:00The 2014 Chemistry Nobel: Beating the Diffraction Limithttp://pipeline.corante.com/archives/2014/10/08/the_2014_chemistry_nobel_beating_the_diffraction_limit.php
This year's Nobel prize in Chemistry goes to Eric Betzig, Stefan Hell, and William Moerner for super-resolution fluorescence microscopy. This was on the list of possible prizes, and has been for several years now (see this comment, which got 2...77366@/home/corante/public_html/pipeline/Chemical News2014-10-08T06:35:54-05:00Molecular Biology Turns Into Chemistryhttp://pipeline.corante.com/archives/2014/10/03/molecular_biology_turns_into_chemistry.php
This is the sort of work that is gradually turning molecular biology into chemistry - and it's a good thing. The authors are studying the movement of a transcription factor protein along a stretch of DNA having two of its...77361@/home/corante/public_html/pipeline/Chemical Biology2014-10-03T06:54:00-05:00Reactive Groups: Still Not So Reactivehttp://pipeline.corante.com/archives/2014/09/08/reactive_groups_still_not_so_reactive.php
Just how reactive are chemical functional groups in vivo? That question has been approached by several groups in chemical biology, notably the Cravatt group at Scripps. One particular paper from them that I've always come back to is this one,...77315@/home/corante/public_html/pipeline/Drug Assays2014-09-08T08:08:55-05:00Proteins Grazing Against Proteinshttp://pipeline.corante.com/archives/2014/08/14/proteins_grazing_against_proteins.php
A huge amount of what's actually going on inside living cells involves protein-protein interactions. Drug discovery, for obvious reasons, focuses on the processes that depend on small molecules and their binding sites (thus the preponderance of receptor ligands and enzyme...77285@/home/corante/public_html/pipeline/Biological News2014-08-14T07:08:43-05:00